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    Novel antibacterial agents
    1.
    发明申请
    Novel antibacterial agents 审中-公开
    新型抗菌剂

    公开(公告)号：US20090111737A1

    公开(公告)日：2009-04-30

    申请号：US12082666

    申请日：2008-04-11

    申请人： Burton G. Christensen ,  Edmund J. Moran ,  John H. Griffin ,  J. Kevin Judice ,  YongQi Mu ,  John L. Pace ,  Mathai Mammen ,  James Aggen

    发明人： Burton G. Christensen ,  Edmund J. Moran ,  John H. Griffin ,  J. Kevin Judice ,  YongQi Mu ,  John L. Pace ,  Mathai Mammen ,  James Aggen

    IPC分类号： A61K38/14 ,  C07K7/00 ,  A61P43/00

    CPC分类号： C07D477/12 ,  C07D499/32 ,  C07D499/44 ,  C07D501/56

    摘要： This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands has a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.

    摘要翻译： 本发明涉及作为抗菌剂的新型多结合化合物（试剂）。 本发明的多相结合化合物包含2-10个配体，其通过连接体或连接体共价连接，其中所述各单体（即，未连接）状态的所述配体具有结合涉及细胞壁生物合成和代谢的酶的能力 用于合成细菌细胞壁和/或细菌细胞表面的前体因而干扰细胞壁的合成和/或代谢。 特别地，本发明的多相结合化合物包含通过接头或接头共价连接的2-10个配体，其中每个所述配体具有能够结合青霉素结合蛋白的配体结构域，转肽酶，转肽酶的底物， β-内酰胺酶，pencillinase酶，头孢菌素酶，转糖基酶或转糖基酶酶底物; 优选地，配体选自β-内酰胺或糖肽类抗菌剂。

    6- and 4-substituted-1-azabicyclo(3.2.0)heptan-3, 7-dione-2-carboxylates
    4.
    发明授权
    6- and 4-substituted-1-azabicyclo(3.2.0)heptan-3, 7-dione-2-carboxylates 失效
    6-和4-取代-1-氮杂双环（3.2.0）庚-3,7-二酮-2-羧酸酯

    公开(公告)号：US4994568A

    公开(公告)日：1991-02-19

    申请号：US481715

    申请日：1990-02-15

    申请人： Burton G. Christensen

    发明人： Burton G. Christensen

    IPC分类号： C07C1/30 ,  C07C17/275 ,  C07C29/147 ,  C07D205/08 ,  C07D477/18 ,  C07F7/10

    CPC分类号： C07F7/10 ,  C07C1/30 ,  C07C17/275 ,  C07C29/147 ,  C07D205/08 ,  C07D477/18 ,  Y02P20/55

    摘要： Disclosed are 6- and 4-substituted-1-azabicyclo[3.2.0]heptan-3,7-dione-2-carboxylic acid esters and salts (I) which are useful in the preparation of 6-, 1- and 2-substituted carbapenem antibiotics. ##STR1## wherein R.sup.5 is a pharmaceutically acceptable ester moiety or a removable protecting group or an alkali or alkaline earth metal cation such as sodium or potassium and wherein R.sup.1, R.sup.2, Rhu 3 and R.sup.4 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, aryl and aralkyl. Another embodiment disclosed is a group of compounds having the formula ##STR2## where X is a leaving group.

    摘要翻译： 公开了6-和4-取代-1-氮杂双环[3.2.0]庚烷-3,7-二酮-2-羧酸酯和盐（I），其可用于制备6-，1-和2- 替代的碳青霉烯类抗生素。 其中R5是药学上可接受的酯部分或可除去的保护基团或碱金属或碱土金属阳离子如钠或钾，并且其中R 1，R 2，R 3和R 4尤其独立地选自 由氢，烷基，芳基和芳烷基组成。 所公开的另一个实施方案是一组具有式“IMAGE”的化合物，其中X是离去基团。

    N-acyl derivatives of thienamycin
    5.
    发明授权
    N-acyl derivatives of thienamycin 失效
    噻吩霉素的N-酰基衍生物

    公开(公告)号：US4839352A

    公开(公告)日：1989-06-13

    申请号：US90400

    申请日：1987-08-27

    申请人： Louis Barash ,  Burton G. Christensen ,  John Hannah ,  William J. Leanza ,  David H. Shih

    发明人： Louis Barash ,  Burton G. Christensen ,  John Hannah ,  William J. Leanza ,  David H. Shih

    IPC分类号： C07D205/08 ,  C07D477/20 ,  C07D498/04

    CPC分类号： C07D477/20 ,  C07D205/08

    摘要： Disclosed are N-acyl derivatives of the antibiotic thienamycin having the following structural formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen and acyl. Such derivatives and their pharmaceutically acceptable salts, are useful as antibiotics. Also disclosed are processes for the preparation of such derivatives, pharmaceutical compositions comprising such derivatives, and methods of treatment comprising administering such derivatives and compositions when an antibiotic effect is indicated.

    摘要翻译： 公开了具有以下结构式的抗生素硫霉素的N-酰基衍生物：其中R 1和R 2独立地选自氢和酰基。 这些衍生物及其药学上可接受的盐可用作抗生素。 还公开了制备这种衍生物的方法，包含这种衍生物的药物组合物，以及治疗方法，包括当指示抗生素效果时施用这样的衍生物和组合物。

    2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids
    6.
    发明授权
    2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids 失效
    2-氮杂取代的1-碳代萘二烯-2-烯-3-羧酸

    公开(公告)号：US4833167A

    公开(公告)日：1989-05-23

    申请号：US743139

    申请日：1985-06-10

    申请人： Burton G. Christensen ,  John C. Chabala ,  Ronald W. Ratcliffe

    发明人： Burton G. Christensen ,  John C. Chabala ,  Ronald W. Ratcliffe

    IPC分类号： C07D477/22 ,  C07F9/6561

    CPC分类号： C07F9/65611 ,  C07D477/22 ,  Y02P20/55

    摘要： Disclosed are 2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids I, where the generic 2-aza group includes azido, acylamino, amino, alkylamino, diaklylamino, triazolyl, triazolinyl, aziridinyl, and their pharmaceutically acceptable salt, ester, anhydride and amide derivatives which are useful as antibiotics. Also disclosed are processes for the preparation of I from the known, appropriately substituted bicyclic keto ester II via the 2-azido central intermediate III: ##STR1## wherein R.sup.16 is H or CH.sub.3, preferably beta-methyl; R.sup.6, and R.sup.7 are independently hydrogen, linear, branched or cyclic C.sub.1 -C.sub.5 alkyl, which can be substituted with fluoro, hydroxy, protected hydroxy, sulfoxy, amino, protected amino wherein R.sup.6 and R.sup.7 taken together can also be C.sub.2 -C.sub.4 alkylidene, similarly substituted; with the proviso that both R.sup.6 and R.sup.7 are not unsubstituted alkyl, R.sup.1 and R.sup.2 are, inter alia, hydrogen, alkyl, acyl, and can be joined to form a ring comprising 3 to 7 atoms; R.sup.a is hydrogen, a salt cation, a removable protecting group, or a pharmaceutically acceptable ester moiety.Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.

    摘要翻译： 公开了2-氮杂取代的1-碳代萘二甲酸-2-烯-3-羧酸I，其中通用2-氮杂基团包括叠氮基，酰氨基，氨基，烷基氨基，二烷基氨基，三唑基，三唑基，氮丙啶基及其药学上可接受的盐 ，酯，酸酐和酰胺衍生物，其可用作抗生素。 还公开了通过2-叠氮中心中间体III从已知的适当取代的双环酮酯II制备I的方法：其中R 16是H或CH 3，优选β-甲基 ; R6和R7独立地是氢，直链，支链或环状的C 1 -C 5烷基，其可以被氟，羟基，保护的羟基，亚磺氧基，氨基，被保护的氨基取代，其中R 6和R 7一起也可以是C 2 -C 4亚烷基 取代 条件是R6和R7都不是未取代的烷基，R1和R2特别是氢，烷基，酰基，并且可以连接形成包含3至7个原子的环; Ra是氢，盐阳离子，可除去的保护基或药学上可接受的酯部分。 还公开了制备这些化合物的方法; 包含这些化合物的药物组合物; 和治疗方法，包括当指出抗生素效应时施用这些化合物和组合物。

    Carbapenems having an internally or externally alkylated mono- or bicyclic 2-quaternary heteroarylalxyl heteromethyl substituent
    7.
    发明授权
    Carbapenems having an internally or externally alkylated mono- or bicyclic 2-quaternary heteroarylalxyl heteromethyl substituent 失效
    具有内部或外部烷基化单环或双环2-季杂芳基甲基取代基的碳青霉烯

    公开(公告)号：US4725594A

    公开(公告)日：1988-02-16

    申请号：US681344

    申请日：1984-12-13

    申请人： Burton G. Christensen ,  James V. Heck ,  Ronald W. Ratcliffe ,  Thomas N. Salzmann

    发明人： Burton G. Christensen ,  James V. Heck ,  Ronald W. Ratcliffe ,  Thomas N. Salzmann

    IPC分类号： C07D487/04 ,  A61K31/40 ,  A61P31/04 ,  C07D477/14

    CPC分类号： C07D477/14

    摘要： Carbapenems having the formula: ##STR1## wherein: R.sup.1 is H;R.sup.4 and R.sup.5 are independently H, CH.sub.3 --, CH.sub.3 CH.sub.2 --, (CH.sub.3).sub.2 CH--, HOCH.sub.2 --, CH.sub.3 CH(OH)--, (CH.sub.3).sub.2 C(OH)--, FCH.sub.2, F.sub.2 CH--, F.sub.3 C--, CH.sub.3 CH(F)--, CH.sub.3 CF.sub.2 --, (CH.sub.3).sub.2 C(F)--; X is --S--, --SO--, --SO.sub.2 --, --O-- or --NH; L is a bridging group comprising substituted or unsubstituted C.sub.1 --C.sub.4 straight, C.sub.2 -C.sub.6 branched or C.sub.3 -C.sub.7 cycloalkyl groups wherein the substituents are selected from C.sub.1 -C.sub.6 alkyl, O--C.sub.1 -C.sub.6 alkyl, S--C.sub.1 -C.sub.6 alkyl, CF.sub.3, N(C.sub.1 -C.sub.6 alkyl).sub.2 ; Y is a carboxy-containing substituent; Het is internally alkylated heteroarylium, ##STR2## or externally alkylated heteroarylium, ##STR3## their preparation and antibiotic use are disclosed.

    摘要翻译： 具有下式的碳青霉烯类：其中：R1是H; （CH 3）2 CH-，HOCH 2 - ，CH 3 CH（OH） - ，（CH 3）2 C（OH） - ，FCH 2，F 2 CH-，F 3 C - ，CH 3 CH（F） - ，CH 3 CF 2 - ，（CH 3）2 C（F） - ; X是-S - ， - SO - ， - SO 2 - ， - O-或-NH; L是包含取代或未取代的C 1 -C 4直链，C 2 -C 6支链或C 3 -C 7环烷基的桥连基团，其中取代基选自C 1 -C 6烷基，O-C 1 -C 6烷基，S-C 1 -C 6烷基，CF 3 ，N（C 1 -C 6烷基）2; Y是含羧基的取代基; Het是内部烷基化杂芳族化合物，图像或外部烷基化杂芳基，其公开了它们的制备和抗生素用途。

    Process for preparing carbapenem compounds
    8.
    发明授权
    Process for preparing carbapenem compounds 失效
    碳青霉烯化合物的制备方法

    公开(公告)号：US4707547A

    公开(公告)日：1987-11-17

    申请号：US859281

    申请日：1986-05-02

    申请人： Burton G. Christensen ,  Ronald W. Ratcliffe

    发明人： Burton G. Christensen ,  Ronald W. Ratcliffe

    IPC分类号： C07D205/08 ,  C07D477/22 ,  C07F7/10 ,  C07F9/6561 ,  C07D487/04 ,  A61K31/40

    CPC分类号： C07D205/08 ,  C07D477/22 ,  C07F7/10 ,  C07F9/65611

    摘要： Disclosed are 6- and 6,6-disubstituted-3-substituted amino-1-azabicyclo[3.2.0]hept-2-en-7-one-2-carboxylic acids (I): ##STR1## wherein R.sup.1 and R.sup.2 are, inter alia, independently selected from the group consisting of hydrogen, substituted and unsubstituted: alkyl, aryl, and aralkyl; and R' and R" are independently selected from the group consisting of: H, substituted and unsubstituted alkyl and aralkyl, or together form a substituted or unsubstituted cyclic group.Such compounds and their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds and methods of treatment comprising administering compounds and compositions when an antibiotic effect is indicated.

    摘要翻译： 公开了6-和6,6-二取代-3-取代的氨基-1-氮杂双环[3.2.0]庚-2-烯-7-酮-2-羧酸（I）：其中R1和R2是 尤其是独立地选自氢，取代和未取代的：烷基，芳基和芳烷基; 并且R'和R“独立地选自：H，取代和未取代的烷基和芳烷基，或一起形成取代或未取代的环状基团。 这些化合物及其药学上可接受的盐，酯和酰胺衍生物可用作抗生素。 还公开了制备这些化合物的方法，包含这些化合物的药物组合物和治疗方法，其中包括当指出抗生素效应时施用化合物和组合物。

    6-(1-hydroxyethyl)-2-carbamimidoyl-pen-2-em-3-carboxylic acids
    9.
    发明授权
    6-(1-hydroxyethyl)-2-carbamimidoyl-pen-2-em-3-carboxylic acids 失效
    6-（1-羟基乙基）-2-氨甲脒基 - 二氧戊环-3-羧酸

    公开(公告)号：US4650794A

    公开(公告)日：1987-03-17

    申请号：US373088

    申请日：1982-04-29

    申请人： Burton G. Christensen ,  Frank P. DiNinno ,  William J. Leanza ,  Ronald W. Ratcliffe

    发明人： Burton G. Christensen ,  Frank P. DiNinno ,  William J. Leanza ,  Ronald W. Ratcliffe

    IPC分类号： C07D499/88 ,  C07D499/00 ,  A61K31/425

    CPC分类号： C07D499/88

    摘要： Disclosed are 6-(1-hydroxyethyl)-2-carbamimidoyl-pen-2-em-3-carboxylic acids (I) having the representative structure: ##STR1## wherein: A is a direct, single bond connecting the indicated S and C atoms, or A is a cyclic or acyclic connecting group selected, inter alia, from alkyl, cycloalkyl, aryl, heteroaryl, heteroalkyl; R.sup.1 and R.sup.2, which define the carbamimidoyl function, are, inter alia, independently selected from hydrogen, alkyl, aryl, alkoxy, amino; additionally, said carbamimidoyl is characterized by cyclic structures achieved by the joinder of the two nitrogen atoms via their substituents and by their joinder to connecting group A; additionally, "carbamimidiums" are disclosed by quaternization of one of the nitrogen atoms of said carbamimidoyl. Such compounds as well as their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.

    摘要翻译： 公开了具有以下代表性结构的6-（1-羟基乙基）-2-氨基甲脒基 - 二-2-甲基-3-羧酸（I）：其中：A是连接所指示的S和 C原子或A是环状或无环连接基团，特别是选自烷基，环烷基，芳基，杂芳基，杂烷基; 定义氨基甲酰基官能团的R 1和R 2尤其独立地选自氢，烷基，芳基，烷氧基，氨基; 另外，所述的氨基甲脒基的特征在于通过两个氮原子通过它们的取代基并通过它们与连接基团A的连接而实现的环状结构; 此外，“氨基甲酰胺”通过所述氨甲脒基的氮原子之一的季铵化来公开。 这些化合物及其药学上可接受的盐，酯和酰胺衍生物可用作抗生素。 还公开了制备这些化合物的方法; 包含这些化合物的药物组合物; 和治疗方法，包括当指出抗生素效应时施用这些化合物和组合物。